Uprima

Impotence is the inability to achieve or maintain the erection necessary to perform sexual intercourse. In the fight against male impotence, a new preparation of Uprima was developed. The main active substance of the tablets is apomorphine hydrochloride. Auxiliary components of the drug are magnesium stearate, microcrystalline cellulose, citric acid, hypromellose, ascorbic acid, disodium edetate, silicon dioxide, iron oxide red (E172), acesulfame potassium, mint-orange flavor, mannitol.

Indications Uprima

The main indications for the use of Uprima are an increase in the activity of the dopaminergic neurotransmitter system of the brain in order to activate sexual interest and exacerbation of sensations in erectile dysfunction.

Release form

The form of Uprima release is sublingual tablets for resorption in 2 mg (pentagonal lozenges) or 3 mg (triangular lozenges), which corresponds to the quantitative content of apomorphine hydrochloride. Red-brown tablets have a double-sided engraving - the letter "a" from one side and the number 2 or 3 from the other.

Pharmacodynamics

Pharmacological action of Uprima is directed to the nuclei of the hypothalamus. This area of the brain is responsible for the production of dopamine, belonging to a group of neurotransmitters and affecting the ability to enjoy. In turn, the paraventricular nucleus of the hypothalamus is a zone where aspects of sexual arousal are concentrated.

Pharmacodynamics of Uprima is due to the properties of apomorphine, the main initiator of erection and sending pro-erectile stimuli. Restoration of erectile function becomes possible due to the normalization of the central nervous system affecting the vascular reactions of the cavernous tissues of the penis.

Pharmacokinetics

The half-life of apomorphine is approximately 3 hours. Oral, intravenous and subcutaneous administration of the drug gives a maximum 2% effect.

Pharmacokinetics of Uprima:

• suction - occurs through the mucosa of the mouth, and after 10 minutes apomorphine appears in the blood plasma (maximum concentration is observed after 40-60 minutes);
• distribution - apomorphine binds to the plasma protein (albumin) by 90%;
• metabolic degradation - is accomplished mainly by conjugation with glucuronic acid or sulfate. The second way of decomposition is through N-demethylation and the creation of Norapomorphine, which is converted into glucuronide and sulfate conjugates;
• Uprima release process - sublingual administration of 2 mg of substance causes the presence of active compounds of apomorphine approximately 90% in urine and 15% in fecal masses. Less than 2% of apomorphine is detected in the urine in an unchanged form. Feces contain apomorphine, norapomorphine and their sulfates.

It should be noted that the pharmacokinetics of Uprima has not been studied in women, as well as in persons under 18 years old. Data on the pharmacokinetics of apomorphine concern healthy men over 65 years of age.

Dosing and administration

The initial dosage of Uprima is prescribed to all patients by 2 mg. The amount of tableted substance is adjusted to a value sufficient to perform sexual intercourse. The value is selected individually, and repeated reception is carried out with an 8-hour interval.

Dosing and Administration:

• immediately before sublingual use, drink a little water, this will help the drug dissolve better;
• approximately 20 minutes before sexual intercourse, place the pill under the tongue;
• The complete dissolution of the drug occurs, usually after 10 minutes. If after 20 minutes the tablet failed to completely dissolve, its residues should be swallowed;
• the effectiveness of the drug is increased by sexual stimulation;
• begin intercourse only when you feel ready for it.

[2]

Use Uprima during pregnancy

Excluded use of Uprima during pregnancy, women, as well as children.

Contraindications

Contraindications to the use of Uprima apply to patients with severe angina pectoris, having a history of myocardial infarction, suffering from heart failure or hypotension, as well as in diseases that limit sexual activity.

The presence of an individual intolerance to one of the components of the drug will also be a ban on its use.

Persons with hepatic insufficiency of various degrees are recommended dosages not higher than 2 mg, subject to strict medical control.

Particular caution should be observed for persons with impaired renal function and anatomical changes in the penis (curvature, cavernous fibrosis, Peyronie's disease, etc.).

Since Uprima can cause dizziness or loss of consciousness, it is not allowed to operate machines and mechanisms for at least 2 hours after taking the medication.

Side effects Uprima

The data of medical observations of a group of 4000 patients of different ages with a diagnosis of erectile dysfunction of organic, psihongennoy or mixed nature, which took 2-3 ml of apomorphine, revealed the side effects of Uprima:

• the ability to develop a vegetative syndrome, manifested by a spontaneous and short-term drop in blood pressure, followed by loss of consciousness (if the dosage is met, the number of cases does not exceed 0.2%);
• deterioration of the general condition, characterized by a pain syndrome of different localization or headaches;
• Reduction of body defenses and susceptibility to infections;
• vasodilation (blood flow in the sense of relaxation of the musculature of the walls of blood vessels and increase of their lumen);
• bouts of nausea;
• drowsiness, loss of consciousness;
• sensation of shortage of air, exacerbation of rhinitis / pharyngitis and increased cough;
• excessive sweating;
• changes in taste.

Receiving Uprima in accordance with the scheme agreed with the expert shows a good tolerance of the drug, and the recorded cases of side effects differ short-term and weak severity.

The drug was tested in patients with hepatic and renal insufficiency, with diabetes mellitus, hypertension, spine traumas and those who underwent prostatectomy. Adverse events with these diseases did not differ in frequency and intensity from other patients.

[1]

Overdose

During the clinical trials, an overdose of Uprima was not detected. Excess dosage of the drug with sublingual administration often causes a vomiting reflex. The use of the drug orally significantly reduces the effect of apomorphine as a result of metabolic degradation.

Proceeding from the fact that there is no specific antidote for apomorphine, in case of an overdose, symptomatic and restorative therapy is prescribed.

The drug should be administered under the control of basic vital signs - blood pressure and heart rate. It is recommended to introduce methods of preventing possible orthostatic hypotension.

In case of severe nausea, blanching of the skin, excessive blood flow or excessive sweating, you should lie on your back and raise your legs. Stay in this position is necessary until the complete disappearance of negative symptoms.

Interactions with other drugs

Conducted analysis of the interaction of Uprima with other drugs (antihypertensive drugs), warns against the simultaneous administration of apomorphine and the introduction of nitrates. Parallel use of drugs with excess dosage of Uprima (more than 5 mg) leads to the occurrence of vasovagal symptoms and a significant reduction in pressure during orthostasis.

Pharmacodynamic interaction of apomorphine in tablets for resorption and agonists / antagonists of dopamine receptors of central action is noted.

The use of alcohol on the background of taking tablets with apomorphine increases the frequency and severity of hypotension. At the same time, alcohol containing drinks leads to a decrease in sexual arousal.

The drug is administered with caution to older men, especially those with uncontrolled hypertension, hypotension or postural hypotension in the history of using antihypertensive drugs.

It is not recommended resorption of tablets of apomorphine with parallel reception of another preparation against impotence.

[3], [4]

Storage conditions

The storage conditions of Uprima in a place protected from direct sunlight and inaccessible to children, subject to a temperature regime up to 25 ° C.

Shelf life

The expiration date of Uprima in unopened packaging is 2 years from the date of manufacture.